Tyrosine kinases inhibitor for c-Kit, PDGFR, and FGFR.
Form:
Free Base
REVIEW Masitinib is a targeted therapy that functions as a receptor tyrosine kinase inhibitor. This small molecule drug inhibits cell signaling by blocking the transfer of phosphate groups at the cell membrane. Masitinib has antitumor properties by selectively inhibiting KIT (also known as stem cell factor) which is a receptor known to be mutated or overactive in many mast cell tumors. Masitinib has antiangiogenic properties through its inhibition of platelet derived growth factor receptor. Interestingly, Masitinib also targets Lyn and Fak, key components of the transduction pathway leading to IgE induced degranulation. This effect expands the possible utility of Masitinib to include atopic disease, an area that has recently completed a clinically successful phase III study.
REFERENCES
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Lublin FD, Reingold SC: Defining the clinical course of multiple sclerosis: results of an international survey. National Multiple Sclerosis Society (USA) Advisory Committee on Clinical Trials of New Agents in Multiple Sclerosis.
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Confavreux C, Vukusic S, Moreau T, Adeleine P: Relapses and progression of disability in multiple sclerosis.
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Thompson AJ, Polman CH, Miller DH, McDonald WI, Brochet B, Filippi MMX, De Sa J: Primary progressive multiple sclerosis.
[4]
Dubreuil P, Letard S, Ciufolini M, Gros L, Humbert M, Casteran N, Borge L, Hajem B, Lermet A, Sippl W, et al.: Masitinib (AB1010), a potent and selective tyrosine kinase inhibitor targeting KIT.
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